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Updated: Jan 29, 2026

Macrophage Differentiation and Polarization into an M2-Like Phenotype using a Human Monocyte-Like THP-1 Leukemia Cell Line
Published on: August 2, 2021
Screening Five Qi-Tonifying Herbs on M2 Phenotype Macrophages.
Yi-Xin Jiang1, Yan Chen2, Yue Yang1
1Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Cailun Road 1200, Shanghai 201203, China.
Total flavonoids from Glycyrrhiza Radix et Rhizoma (TFRG) and other Qi-tonifying herbs inhibit M2 macrophage polarization, a key factor in cancer progression. This research identifies natural products for potential cancer immune therapy by regulating the tumor microenvironment.
Area of Science:
- Immunology
- Pharmacology
- Traditional Chinese Medicine
Background:
- Tumor-associated macrophages (TAMs) with an M2 phenotype are crucial in the tumor microenvironment (TME) and linked to poor cancer prognosis.
- Regulating TAM polarization presents a promising strategy for cancer immune therapy.
Purpose of the Study:
- To screen Qi-tonifying herbs from Traditional Chinese Medicine (TCM) for their ability to inhibit M2 macrophage polarization.
- To investigate the molecular mechanisms of promising candidates, particularly total flavonoids from Glycyrrhiza Radix et Rhizoma (TFRG).
Main Methods:
- Screening of extracts and ingredients from five Qi-tonifying herbs for inhibition of M2 polarization in murine macrophages (RAW264.7) induced by IL-4 and IL-13.
- Assessing the expression of M2 markers (Arginase-1, FIZZ1, YM1, CD206) and M1 marker (iNOS).
- Investigating the effects of TFRG on STAT6 phosphorylation and miR-155 expression.
Main Results:
- Total flavonoids from Glycyrrhiza Radix et Rhizoma (TFRG) and Ginseng Radix et Rhizoma significantly inhibited Arginase-1 (Arg-1) expression.
- TFRG suppressed M2 macrophage migration, reduced M2 marker expression, and increased M1 marker expression.
- TFRG decreased STAT6 phosphorylation and increased miR-155 expression, indicating a mechanism for regulating M1/M2 polarization.
Conclusions:
- Several Qi-tonifying herbs and their components show potential for inhibiting M2 macrophage polarization.
- TFRG is a promising candidate for cancer immune therapy, acting partly by inactivating the STAT6 pathway and modulating miR-155.
- This study provides natural products for immune regulation in the tumor microenvironment.
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